|
|
| (12 intermediate revisions not shown.) |
| Line 1: |
Line 1: |
| - | [[Image:2c5p.gif|left|200px]]<br /> | + | #REDIRECT [[2wev]] This PDB entry is obsolete and replaced by 2wev |
| - | <applet load="2c5p" size="450" color="white" frame="true" align="right" spinBox="true"
| + | |
| - | caption="2c5p, resolution 2.30Å" />
| + | |
| - | '''DIFFERENTIAL BINDING OF INHIBITORS TO ACTIVE AND INACTIVE CDK2 PROVIDES INSIGHTS FOR DRUG DESIGN'''<br />
| + | |
| - | | + | |
| - | ==Overview==
| + | |
| - | The cyclin-dependent kinases (CDKs) have been characterized in complex, with a variety of inhibitors, but the majority of structures solved are in, the inactive form. We have solved the structures of six inhibitors in both, the monomeric CDK2 and binary CDK2/cyclinA complexes and demonstrate that, significant differences in ligand binding occur depending on the, activation state. The binding mode of two ligands in particular varies, substantially in active and inactive CDK2. Furthermore, energetic analysis, of CDK2/cyclin/inhibitors demonstrates that a good correlation exists, between the in vitro potency and the calculated energies of interaction, but no such relationship exists for CDK2/inhibitor structures. These, results confirm that monomeric CDK2 ligand complexes do not fully ... [[http://ispc.weizmann.ac.il/pmbin/getpm?16492568 (full description)]]
| + | |
| - | | + | |
| - | ==About this Structure==
| + | |
| - | 2C5P is a [[http://en.wikipedia.org/wiki/Protein_complex Protein complex]] structure of sequences from [[http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]] with CK7 as [[http://en.wikipedia.org/wiki/ligand ligand]]. Active as [[http://en.wikipedia.org/wiki/Transferred_entry:_2.7.11.1 Transferred entry: 2.7.11.1]], with EC number [[http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.1.37 2.7.1.37]]. Structure known Active Site: AC1. Full crystallographic information is available from [[http://ispc.weizmann.ac.il/oca-bin/ocashort?id=2C5P OCA]].
| + | |
| - | | + | |
| - | ==Reference==
| + | |
| - | Differential binding of inhibitors to active and inactive CDK2 provides insights for drug design., Kontopidis G, McInnes C, Pandalaneni SR, McNae I, Gibson D, Mezna M, Thomas M, Wood G, Wang S, Walkinshaw MD, Fischer PM, Chem Biol. 2006 Feb;13(2):201-11. PMID:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=16492568 16492568]
| + | |
| - | [[Category: Homo sapiens]]
| + | |
| - | [[Category: Protein complex]]
| + | |
| - | [[Category: Transferred entry: 2.7.11.1]]
| + | |
| - | [[Category: Fischer, P.M.]]
| + | |
| - | [[Category: Gibson, D.]]
| + | |
| - | [[Category: Imcnae]]
| + | |
| - | [[Category: Kontopidis, G.]]
| + | |
| - | [[Category: Mcinnes, C.]]
| + | |
| - | [[Category: Mezna, M.]]
| + | |
| - | [[Category: Pandalaneni, S.R.]]
| + | |
| - | [[Category: Thomas, M.]]
| + | |
| - | [[Category: Walkinshaw, M.D.]]
| + | |
| - | [[Category: Wang, S.]]
| + | |
| - | [[Category: Wood, G.]]
| + | |
| - | [[Category: CK7]]
| + | |
| - | [[Category: atp-binding]]
| + | |
| - | [[Category: cdk2]]
| + | |
| - | [[Category: cell cycle]]
| + | |
| - | [[Category: cell division]]
| + | |
| - | [[Category: cyclin]]
| + | |
| - | [[Category: differential inhibition]]
| + | |
| - | [[Category: kinase]]
| + | |
| - | [[Category: mitosis]]
| + | |
| - | [[Category: nucleotide-binding]]
| + | |
| - | [[Category: phosphorylation]]
| + | |
| - | [[Category: polymorphism]]
| + | |
| - | [[Category: serine/threonine-protein]]
| + | |
| - | [[Category: transferase]]
| + | |
| - | | + | |
| - | ''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Tue Oct 30 13:36:59 2007''
| + | |
